R-R-VVD-118313-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(R,R)-VVD-118313Cat.No.:HY-151385ACASNo.:2875046-31-2分?式:C??H??Cl?N?O?S分?量:429.36作?靶點(diǎn):STAT;InterleukinRelated;IFNAR;JAK作?通路:JAK/STATSignaling;StemCell/Wnt;Immunology/Inflammation;Epigenetics;ProteinTyrosineKinase/RTK儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(232.90mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3290mL11.6452mL23.2905mL5mM0.4658mL2.3290mL4.6581mL10mM0.2329mL1.1645mL2.3290mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性(R,R)-VVD-118313VVD-118313(HY-151385)的異構(gòu)體。VVD-118313?種選擇性JAK1抑制劑，可阻斷JAK1依賴的反式磷酸化和細(xì)胞因?信號(hào)。VVD-118313可?于癌癥的研究。IC50&TargetJAK11/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究VVD-118313(compound5a;0.01-10?μM;3h;primaryhumanPBMCs)inhibitsJAK1byengagementofC817andJAK2byengagementofC838.VVD-118313inhibitscysteinereactivityinadose-dependentmanner[1].VVD-118313(2μM,2h)blocksIFNα-simulatedSTAT1andIL-6-stimulatedSTAT3phosphorylationinWT-orC810A-JAK1-expressing22Rv1cells.VVD-118313alsoblockstheconstitutivephosphorylationofWT-andC810A-JAK1[1].VVD-118313(0.01-10?μM)selectivelyinhibitsJAK1signalinginprimaryhumanimmunecells.VVD-118313inhibitsJAK1-dependentIFNα-pSTAT1,IL-6-pSTAT3,andIL-2-pSTAT5pathwaysinhumanPBMCsinadose-dependentmanner[1].VVD-118313(0.1-0.4μM;24h)inhibitsT-cellactivationinduction.VVD-118313inhibitstheactivationofhumanTcellsco-stimulatedwithαCD3/αCD28byareductionintheproportionofCD25+Tcells.VVD-118313blocksthesecretionoftheTh1-polarizingcytokineIFNγandincreasestheproductionofIL-2[1].VVD-118313(0.1-0.5?μM;2h)inhibitsontheproductionofpro-inflammatorycytokinesandchemokines.VVD-118313suppressestheinductionofseveralpro-inflammatorychemokines,includingCCL2/MCP-1,CXCL10/IP-10,andCCL4/MIP-1β[1].WesternBlotAnalysis[1]CellLine:22Rv1cellsConcentration:0.01,0.1,and1μMIncubationTime:2hoursResult:ShowedlabelingofrecombinantWT-JAK1andC810A-JAK1,butnotC817A-JAK1.InhibitedWT-andC810A-JAK1phosphorylationwithevengreaterpotencythanSTAT1/STAT3phosphorylation.體內(nèi)研究VVD-118313(compound5a;25-50mg/kg;i.h.;once)inhibitsJAK1signalinginTYK2knockoutmice[1].REFERENCES[1].KavanaghME,et,al.SelectiveinhibitorsofJAK1targetinganisoform-restrictedallostericcysteine.NatChemBiol.2022Sep12.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica